Apigenin and Hypertension: A Review of Natural Sources, Pharmacodynamic and Pharmacokinetic Evidence.

PURPOSE: This review aimed to synthesize recent evidence on the pharmacological effects of APG in the management of hypertension.

METHODS

A comprehensive literature search was conducted using PubMed, Scopus, Web of Science, and Google Scholar.

RESULTS

Pharmacokinetic studies reveal that APG exhibits poor oral bioavailability due to low solubility and extensive metabolism yet demonstrates wide tissue distribution and neuroprotective potential. It interacts with drug-metabolizing enzymes and transporters, influencing the pharmacokinetics of co-administered agents while maintaining a favorable safety profile at dietary levels. Preclinical evidence shows that APG lowers blood pressure by promoting vasodilation through TRPV4/NO pathways, attenuating oxidative stress and inflammation, and regulating genetic signaling to prevent vascular and cardiac remodeling. Toxicity studies confirm safety up to 5000 mg/kg, while additional findings highlight its beneficial modulation of gut microbiota.

CONCLUSION

APG emerges as a promising supplementary compound for hypertension management, combining vascular, molecular, and microbiome-mediated mechanisms with a strong safety margin.